CN105051039A - 喹唑啉衍生物的固态形式及其作为braf抑制剂的用途 - Google Patents

喹唑啉衍生物的固态形式及其作为braf抑制剂的用途 Download PDF

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Publication number
CN105051039A
CN105051039A CN201480011572.8A CN201480011572A CN105051039A CN 105051039 A CN105051039 A CN 105051039A CN 201480011572 A CN201480011572 A CN 201480011572A CN 105051039 A CN105051039 A CN 105051039A
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China
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degree
compound
crystal formation
peak
ray powder
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CN201480011572.8A
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English (en)
Chinese (zh)
Inventor
斯蒂芬·J·比尔迈尔
拉尔夫·C·霍尔蒂万格
马丁·J·雅各布斯
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Ignyta Inc
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Ignyta Inc
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Publication of CN105051039A publication Critical patent/CN105051039A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/08—Malonic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201480011572.8A 2013-03-11 2014-03-11 喹唑啉衍生物的固态形式及其作为braf抑制剂的用途 Pending CN105051039A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361776081P 2013-03-11 2013-03-11
US61/776,081 2013-03-11
PCT/US2014/023110 WO2014164648A2 (en) 2013-03-11 2014-03-11 Solid state forms of a quinazoline derivative and its use as a braf inhibitor

Publications (1)

Publication Number Publication Date
CN105051039A true CN105051039A (zh) 2015-11-11

Family

ID=50771322

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480011572.8A Pending CN105051039A (zh) 2013-03-11 2014-03-11 喹唑啉衍生物的固态形式及其作为braf抑制剂的用途

Country Status (15)

Country Link
US (3) US9353097B2 (de)
EP (1) EP2956454A2 (de)
JP (1) JP2016512516A (de)
KR (1) KR20150132118A (de)
CN (1) CN105051039A (de)
AU (2) AU2014249158B2 (de)
BR (1) BR112015022207A8 (de)
CA (1) CA2901204C (de)
EA (1) EA025561B1 (de)
HK (2) HK1217193A1 (de)
IL (1) IL241239A0 (de)
MX (1) MX2015012318A (de)
NZ (1) NZ710600A (de)
TW (1) TW201512192A (de)
WO (1) WO2014164648A2 (de)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110191705A (zh) * 2016-12-01 2019-08-30 亚尼塔公司 治疗癌症的方法
CN111153860A (zh) * 2019-12-30 2020-05-15 广州六顺生物科技股份有限公司 一种喹唑啉类化合物的晶型及其制备方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015012318A (es) 2013-03-11 2016-04-15 Ignyta Inc Formas de estado solido de un derivado de quinazolina y su uso como un inhibidor de braf.
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070244120A1 (en) * 2000-08-18 2007-10-18 Jacques Dumas Inhibition of raf kinase using substituted heterocyclic ureas
CN102026985A (zh) * 2008-03-17 2011-04-20 埃姆比特生物科学公司 喹唑啉衍生物作为raf激酶调节剂以及它们的方法和用途
WO2012138783A2 (en) * 2011-04-04 2012-10-11 Netherlands Cancer Institute Methods and compositions for predicting resistance to anticancer treatment

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015012318A (es) 2013-03-11 2016-04-15 Ignyta Inc Formas de estado solido de un derivado de quinazolina y su uso como un inhibidor de braf.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070244120A1 (en) * 2000-08-18 2007-10-18 Jacques Dumas Inhibition of raf kinase using substituted heterocyclic ureas
CN102026985A (zh) * 2008-03-17 2011-04-20 埃姆比特生物科学公司 喹唑啉衍生物作为raf激酶调节剂以及它们的方法和用途
WO2012138783A2 (en) * 2011-04-04 2012-10-11 Netherlands Cancer Institute Methods and compositions for predicting resistance to anticancer treatment

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JOYCE JAMES，等: "CEP-32496:A Novel Orally Active BRAF(V600E) Inhibitor with Selective Cellular and In Vivo Antitumor Activity", 《MOLECULAR CANCER THERAPEUTICS》 *
MARTIN W. ROWBOTTOM，等: "Identification of1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride(CEP-32496),a HighlyPotent and Orally Efficacious Inhibitor ofV-RAF Murine Sarcoma ViralOncogene HomologueB1(BRAF)V600E", 《JOURNAL OF MEDICINAL CHEMISTRY》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110191705A (zh) * 2016-12-01 2019-08-30 亚尼塔公司 治疗癌症的方法
CN111153860A (zh) * 2019-12-30 2020-05-15 广州六顺生物科技股份有限公司 一种喹唑啉类化合物的晶型及其制备方法
CN111153860B (zh) * 2019-12-30 2021-06-29 广州六顺生物科技股份有限公司 一种喹唑啉类化合物的晶型及其制备方法

Also Published As

Publication number Publication date
US20160280698A1 (en) 2016-09-29
KR20150132118A (ko) 2015-11-25
BR112015022207A2 (pt) 2017-07-18
US9718810B2 (en) 2017-08-01
US9987281B2 (en) 2018-06-05
HK1217333A1 (zh) 2017-01-06
US20170290833A1 (en) 2017-10-12
MX2015012318A (es) 2016-04-15
WO2014164648A2 (en) 2014-10-09
AU2016204294B9 (en) 2017-09-21
EA201591259A1 (ru) 2016-02-29
AU2014249158B2 (en) 2016-07-28
EP2956454A2 (de) 2015-12-23
WO2014164648A3 (en) 2014-11-27
TW201512192A (zh) 2015-04-01
CA2901204A1 (en) 2014-10-09
AU2016204294B2 (en) 2017-08-31
US9353097B2 (en) 2016-05-31
AU2014249158A1 (en) 2015-09-17
CA2901204C (en) 2018-07-10
IL241239A0 (en) 2015-11-30
WO2014164648A4 (en) 2015-01-29
EA025561B1 (ru) 2017-01-30
HK1217193A1 (zh) 2016-12-30
JP2016512516A (ja) 2016-04-28
US20150376171A1 (en) 2015-12-31
NZ710600A (en) 2017-01-27
AU2016204294A1 (en) 2016-07-14
BR112015022207A8 (pt) 2018-01-23

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